Process for preparing pyrimidone derivatives

Details Process for preparing pyrimidone derivatives Process for preparing pyrimidone derivatives

C - Chemistry, Metallurgy

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D

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C07D 401/12 (2006.01) C07D 213/38 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01)

Patent

CA 1170261

11740 ABSTRACT New Compounds (1) Image (1) in which R1 and R2 are C1-C4 alkyl or together with the nitrogen atom to which they are attached form a pyrrolidino or piperidino group; Y is methylene or sulphur; X is methylene or oxygen provided that X is methylene when Y is sulphur; Z is hydrogen or C1-C4 alkyl; and R5 is hydrogen, C1-C4 alkyl or -A-B where A is C1-C4 alkylene and B is optionally substituted heteroaryl or phenyl. are prepared by reacting an amine (2) with a pyrimidone (3) (in which Q is nitroamino, lower alkylthio, benzylthio, chlorine, bromine or other group which can be displaced with a primary amine and R has the same significance as R5 or can be a protected derivative of the group -A-B), removing any protecting group present, Image Image (2) (3) 11740 or by reacting a guanidine (4) with a .beta.-oxoester (5) Image Image (4) (5) or where X is methylene and Y is sulphur by reacting a compound (6) (in which L is a group displaceable with a thiol)with a compound (7). The compounds (1) are useful as histamine H2-antagonists. Image Image (6) (7)

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